Institute of Pharmacy and Molecular Biotechnology, Heidelberg University, Im Neuenheimer Feld 364, 69120 Heidelberg, Germany.
Chin Med. 2014 Jan 17;9(1):4. doi: 10.1186/1749-8546-9-4.
Bupleurum marginatum Wall. ex DC (Apiaceae) is a perennial herb widely used in traditional Chinese and Kampo medicine for the treatment of various infectious diseases. The biological activities of B. marginatum have not been fully investigated. This study aims to investigate the antitrypanosomal, antimicrobial and antiviral activities of methanol (ME) and dichloromethane (DCM) extracts of B. marginatum aerial parts and the ability of both extracts to inhibit the growth of different cancer cell lines.
Phytochemical characterization of the extracts was performed by LC-MS profiling. The antitrypanosomal activity was evaluated using the resazurin method. The antimicrobial activity was assessed using agar diffusion and microdilution methods, and the minimum inhibitory concentration (MIC) values were determined. The antiviral activity was determined for 6.25, 12.5, and 50 μg/mL doses using a plaque reduction assay. Cytotoxicity was investigated in eight cancer cell lines (Caco-2, CCL-81, CCRF-CEM, COS-7, HL-60, MIA PaCa-2, MCF-7, and PANC-1) using the MTT assay and the caspase 3/7 activity was determined over the range of 62.5-1000 μg/mL.
Phytochemical analyses resulted in the characterization of 15 components, mainly flavonoids and lignans. The DCM extract showed significant antitrypanosomal activity (IC50: 36.21 μg/mL) and moderate activity against Streptococcus pyogenes (MIC value: 0.25 mg/mL). At a dose of 12.5 μg/mL, the DCM extract inhibited 73.6% of the plaque production by hepatitis A virus. CCRF-CEM cells were the most sensitive to both extracts (IC50: 12.5-22.7 μg/mL). The cytotoxicity was mediated by induction of apoptosis (19-fold increase in the cellular caspase 3/7 level after treatment with the DCM extract at 1 mg/mL).
ME and DCM extract of B. marginatum showed anti-infective and antiproliferative effects.
柴胡（伞形科）是一种多年生草本植物，广泛用于中药和汉方医学治疗各种传染病。柴胡的生物活性尚未得到充分研究。本研究旨在探讨柴胡地上部分甲醇（ME）和二氯甲烷（DCM）提取物的抗锥虫、抗菌和抗病毒活性，以及两种提取物抑制不同癌细胞系生长的能力。
采用 LC-MS 谱法对提取物进行植物化学特征分析。采用 Resazurin 法评价抗锥虫活性。采用琼脂扩散和微量稀释法评价抗菌活性，测定最小抑菌浓度（MIC）值。采用噬斑减少法测定 6.25、12.5 和 50μg/mL 剂量的抗病毒活性。采用 MTT 法在八种癌细胞系（Caco-2、CCL-81、CCRF-CEM、COS-7、HL-60、MIA PaCa-2、MCF-7 和 PANC-1）中测定细胞毒性，测定细胞内 caspase 3/7 活性在 62.5-1000μg/mL 范围内的变化。
植物化学分析结果表明，主要成分为黄酮类和木脂素类化合物 15 种。DCM 提取物对锥虫有显著的抗活性（IC50：36.21μg/mL），对化脓性链球菌（MIC 值：0.25mg/mL）也有中等活性。DCM 提取物在 12.5μg/mL 剂量下，可抑制甲型肝炎病毒 73.6%的蚀斑形成。两种提取物对 CCRF-CEM 细胞最为敏感（IC50：12.5-22.7μg/mL）。细胞毒性是通过诱导细胞凋亡介导的（DCM 提取物在 1mg/mL 时，细胞 caspase 3/7 水平增加 19 倍）。
柴胡的 ME 和 DCM 提取物具有抗感染和抗增殖作用。
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